CO6150172A2 - INHIBITORS OF THE METALOPROTEINASE MATRIX - Google Patents

INHIBITORS OF THE METALOPROTEINASE MATRIX

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Publication number
CO6150172A2
CO6150172A2 CO09017757A CO09017757A CO6150172A2 CO 6150172 A2 CO6150172 A2 CO 6150172A2 CO 09017757 A CO09017757 A CO 09017757A CO 09017757 A CO09017757 A CO 09017757A CO 6150172 A2 CO6150172 A2 CO 6150172A2
Authority
CO
Colombia
Prior art keywords
heteroaryl
nhc
nr4r5
aralkyl
alkyl
Prior art date
Application number
CO09017757A
Other languages
Spanish (es)
Inventor
Viswajanai Jitendra Sattigeri
Venkata P Palle
Manoj Kumar Khera
Ranadheer Reddy
Manoj Kumar Tiwari
Ajay Soni
Adbul Rehman Rauf
Sony Joseph
Arpita Musib
Sunanda Dastidar
Punit Kumar Srivastava
Original Assignee
Ranbaxy Lab Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ranbaxy Lab Ltd filed Critical Ranbaxy Lab Ltd
Publication of CO6150172A2 publication Critical patent/CO6150172A2/en

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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  • Enzymes And Modification Thereof (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

1.- Un compuesto de la Fórmula I:en donde: * representa un centro asimétrico estereogénico de configuración definida seleccionada de (R, R) , (S, S) (R, S) y (S,R) ; n es un entero de 1 a 5; R1 es hidrógeno, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, heteroarilo, aralquilo, alcoxi, ariloxi, alqueniloxi o alquiniloxi opcionalmente sustituido; R2 es heterociclilo, heteroarilo, NR4R5, -NHC(=Y)R4, -NHC(=Y)NR5Rx, -NHC(=O)OR4, -NHSO2R4, C(=Y)NR4R5, C(=O)OR6, en donde: Y es oxígeno o azufre, OR5, -OC(=O)NR4R5, O-acilo, S(O)mR4, -SO2N(R4)2, ciano, amidino o guanidino; Rx es R4 o -SO2N(R4)2;R6 es hidrógeno, alquilo, cicloalquilo, aralquilo, heteroarilalquilo, heterociclilalquilo o cicloalquilalquilo en donde:R4 es alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, heteroarilo, aralquilo, heteroarilalquilo, heterociclilalquilo o cicloalquilalquilo; y m es un entero 0-2; R5 es hidrógeno o R4;R3 es hidrógeno, fluor, alquilo, cicloalquilalquilo o aralquilo; A es OH, OR4, -OC(=O)NR4R5, O-acilo, NH2, NR4R5, -NHC(=Y)R4, -NHC(=Y)NR5Rx, -NHC(=O)OR4, -NHSO2R4; Q es arilo o heteroarilo opcionalmente sustituido.1.- A compound of Formula I: where: * represents a stereogenic asymmetric center of defined configuration selected from (R, R), (S, S) (R, S) and (S, R); n is an integer from 1 to 5; R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, alkoxy, aryloxy, alkenyloxy or optionally substituted alkynyloxy; R2 is heterocyclyl, heteroaryl, NR4R5, -NHC (= Y) R4, -NHC (= Y) NR5Rx, -NHC (= O) OR4, -NHSO2R4, C (= Y) NR4R5, C (= O) OR6, in where: Y is oxygen or sulfur, OR5, -OC (= O) NR4R5, O-acyl, S (O) mR4, -SO2N (R4) 2, cyano, amidino or guanidino; Rx is R4 or -SO2N (R4) 2; R6 is hydrogen, alkyl, cycloalkyl, aralkyl, heteroarylalkyl, heterocyclylalkyl or cycloalkylalkyl wherein: R4 is alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, heteroaryl, aralkyl, heteroaryl, heteroaryl, heteroaryl, heteroaryl or cycloalkylalkyl; and m is an integer 0-2; R5 is hydrogen or R4; R3 is hydrogen, fluorine, alkyl, cycloalkylalkyl or aralkyl; A is OH, OR4, -OC (= O) NR4R5, O-acyl, NH2, NR4R5, -NHC (= Y) R4, -NHC (= Y) NR5Rx, -NHC (= O) OR4, -NHSO2R4; Q is optionally substituted aryl or heteroaryl.

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